| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
TTA-A2 demonstrated state-inhibitory suppression of α1I in typical voltage-clamp electrophysiological experiments, with effects of 98 nM and 3.7 μM, respectively, at membrane holding potentials of -80 and -100 mV. Moreover, shows excellent selectivity for hERG potassium channels and L-type calcium channels (IC50>10μM)[1] and high affinity Ki of 1.2 nM in α1I binding for Cav1.2 (L-type), Cav2.1 (P/Q-type), Cav2.2 (N-type), and Cav2.3 (R-type) channels with IC >30 μM, 80 mV.
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|---|---|
| ln Vivo |
A single dosage of TTA-A2 (gavage; 3 mg/kg) significantly alters the architecture of reserve sleep. Active arousal declines shortly after carbon dioxide exposure, but delta and REM sleep rise and decrease, respectively. Additionally, TTA-A2 (gavage; 10 mg/kg; once daily; 5 days) showed these effects during sleep. In wild-type mice, TTA-A2 reduces voluntary arousal and promotes deep sleep by exhibiting periodic effects on periodic thalamocortical network activity. Wave sleep does not affect mice deficient in Cav3.1 or Cav3.3, albeit [2].
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| Animal Protocol |
Animal/Disease Models: wild-type and dual Cav3.1/Cav3.3 knockout C57BL6/Sv129 background mice [2]
Doses: 10 mg/kg Route of Administration: po (oral gavage); 10 mg/kg; one time/day; 5-day Experimental Results: Prevents active arousal and promotes slow-wave sleep in wild-type mice, but not in mutant mice. |
| References |
| Molecular Formula |
C20H21F3N2O2
|
|---|---|
| Molecular Weight |
378.4
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| Exact Mass |
378.155
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| CAS # |
953778-63-7
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| PubChem CID |
53317097
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
538.5±50.0 °C at 760 mmHg
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| Flash Point |
279.5±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.545
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| LogP |
3.58
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
488
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](C1=NC=C(C=C1)OCC(F)(F)F)NC(=O)CC2=CC=C(C=C2)C3CC3
|
| InChi Key |
GEYDMBNDOVPFJL-CYBMUJFWSA-N
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| InChi Code |
InChI=1S/C20H21F3N2O2/c1-13(18-9-8-17(11-24-18)27-12-20(21,22)23)25-19(26)10-14-2-4-15(5-3-14)16-6-7-16/h2-5,8-9,11,13,16H,6-7,10,12H2,1H3,(H,25,26)/t13-/m1/s1
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| Chemical Name |
2-(4-cyclopropylphenyl)-N-[(1R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethyl]acetamide
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| Synonyms |
TTA-A2; TTA A2; TTAA2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~264.28 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.61 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6427 mL | 13.2135 mL | 26.4271 mL | |
| 5 mM | 0.5285 mL | 2.6427 mL | 5.2854 mL | |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6427 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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